CAS: 149647-78-9; N1-Hydroxy-N8-Phenyloctanediamide

该化合物是一种甲型脱乙酰酶抑制剂(HDACi),有选择地针对HDAC2, 调节基因表达方式和抑制各种癌症细胞类型的扩散. 这种复合物显示出强大的抗扩散活动,并显示出通过诱导差异和吸附性来治疗诸如皮肤T细胞淋巴瘤等血性恶性肿瘤的希望.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号149648-52-2 7-苯基氨基甲酰基庚酸 | CAS号162853-41-0 8-氧代-8-(苯基氨基)辛酸甲酯 | CAS号505-48-6 辛二酸 | CAS号149647-86-9 8-(hydroxyamino... | CAS号3946-32-5 辛二酸单甲酯 | CAS号10521-06-9 氧杂蒽酮-2,9-二酮

合成工艺路线路线简述

    Ethoxycarbonyl 8-Anilino-8-Oxooctanoate置于盐酸羟胺体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 1.5H,反应生成伏立诺他
    参考文献:纳米递送的伏立诺他衍生物是一种有前景的用于治疗内脏利什曼病的口服化合物
    标题:纳米递送的伏立诺他衍生物是一种有前景的用于治疗内脏利什曼病的口服化合物
    摘要:目前尚无令人满意的内脏利什曼病治疗方法.因此该病急需新药.理想的候选人应该是有效,安全,负担得起的,并且可以通过口服途径进行管理.组蛋白脱乙酰基酶(hdacs)参与沉默关键的调控途径,包括促凋亡程序,并且代表了药物干预的潜在治疗靶标.传统上认为o-烷基异羟肟酸酯对哺乳动物hdac没有作用.这项研究的目的是评估mdg(o的saha衍生物)的作用-烷基异羟肟酸酯家族,对人组蛋白脱乙酰基酶,内脏利什曼病致病因子和小鼠模型无活性.还评估了伏立诺他,Tubacin和丙戊酸(众所周知的哺乳动物hdac抑制剂)对寄生虫的影响.发现mdg在体外对婴儿利什曼原虫和杜氏利什曼原虫细胞内的变形虫具有很高的活性,但对前鞭毛体阶段却没有活性.相反,伏立诺他,Tubacin和丙戊酸对寄生虫没有活性.体外研究herg和cav1.2通道的检测方法没有发现mdg驱动的心脏毒性的证据.Mdg既没有显示出肝毒性也没有诱变性,也
    Doi:10.1016/j.Phrs.2018.11.039

    海关参考信息

    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:WO-2017100796-A1
    优先权日:2015-12-11
    标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
    权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

    专利号:US-2025235415-A1
    优先权日:2022-02-23
    标 题:Modulation of human breast milk composition
    发明人:ROSS MICHAEL G; DESAI MINA
    权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER
    摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
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    主要参考文献


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    合成参考文献


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    摘要:Luo Y, Liu HM, Su MB, Sheng L, Zhou YB, Li J, Lu W. Synthesis and biological evaluation of piperamide analogues as HDAC inhibitors. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4844–6. doi: 10.1016/j.bmcl.2011.06.046.
    参考文献:10.1158/1535-7163.mct-10-1108
    摘要:Dasmahapatra G, Lembersky D, Son MP, Attkisson E, Dent P, Fisher RI, Friedberg JW, Grant S. Carfilzomib Interacts Synergistically with Histone Deacetylase Inhibitors in Mantle Cell Lymphoma Cells In Vitro and In Vivo. 2011 Sep 01;10(9):1686–97. doi: 10.1158/1535-7163.mct-10-1108.
    参考文献:10.1111/j.1600-0609.2011.01683.x
    摘要:Corazzelli G, Frigeri F, Arcamone M, Aloj L, Capobianco G, Becchimanzi C, Morelli E, Volzone F, Marcacci G, Russo F, De Filippi R, Lastoria S, Pinto A. Efficacy and safety of the third-generation chloroethylnitrosourea fotemustine for the treatment of chemorefractory T-cell lymphomas. Eur J Haematol. 2011 Dec;87(6):547–53.
    参考文献:10.1002/pmic.201100092
    摘要:Bianchi L, Bruzzese F, Leone A, Gagliardi A, Puglia M, Di Gennaro E, Rocco M, Gimigliano A, Pucci B, Armini A, Bini L, Budillon A. Proteomic analysis identifies differentially expressed proteins after HDAC vorinostat and EGFR inhibitor gefitinib treatments in Hep-2 cancer cells. Proteomics. 2011 Sep;11(18):3725–42. doi: 10.1002/pmic.201100092.
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